Osimertinib (AZD9291) and CNS Response in Two Radiotherapy-Naïve Patients with EGFR-Mutant and T790M-Positive Advanced Non-Small Cell Lung Cancer

Clin Drug Investig. 2016 Aug;36(8):683-6. doi: 10.1007/s40261-016-0411-1.

Abstract

The discovery of sensitizing epidermal growth factor receptor (EGFR) mutations as a predictive marker of sensitivity to first-generation EGFR tyrosine kinase inhibitors (TKIs) has dramatically changed the paradigm of care for advanced non-small cell lung cancer (NSCLC) patients. Unfortunately, the majority of patients with EGFR-mutant NSCLC treated with EGFR-TKIs develop acquired resistance within 14-16 months. T790M mutation recently emerged as a major determinant of acquired resistance to gefitinib and erlotinib. Osimertinib (AZD9291) is a novel mono-anilino-pyrimidine third-generation EGFR TKI targeting both sensitizing and T790M EGFR-mutation which showed promising results in T790M-positive NSCLC. Here we report two cases of gefitinib- or erlotinib-pretreated NSCLCs with a T790M mutation-positive (as assessed on plasma through the therascreen EGFR test) disease and untreated, asymptomatic central nervous system metastases that responded to treatment with osimertinib.

MeSH terms

  • Acrylamides
  • Aged
  • Aniline Compounds
  • Antineoplastic Agents / therapeutic use*
  • Brain / diagnostic imaging
  • Carcinoma, Non-Small-Cell Lung / drug therapy*
  • Carcinoma, Non-Small-Cell Lung / genetics*
  • Carcinoma, Non-Small-Cell Lung / pathology
  • Central Nervous System Neoplasms / prevention & control*
  • Central Nervous System Neoplasms / secondary*
  • Drug Resistance, Neoplasm / genetics
  • ErbB Receptors / genetics*
  • Female
  • Humans
  • Lung Neoplasms / drug therapy*
  • Lung Neoplasms / genetics*
  • Lung Neoplasms / pathology
  • Magnetic Resonance Imaging
  • Male
  • Middle Aged
  • Neoplasm Metastasis / prevention & control
  • Piperazines / therapeutic use*
  • Protein Kinase Inhibitors / therapeutic use*
  • Treatment Outcome

Substances

  • Acrylamides
  • Aniline Compounds
  • Antineoplastic Agents
  • Piperazines
  • Protein Kinase Inhibitors
  • osimertinib
  • EGFR protein, human
  • ErbB Receptors